LOCAMETZ
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LOCAMETZ (LOCAMETZ).
Metformin hydrochloride is a biguanide antihyperglycemic agent that improves glucose tolerance in patients with type 2 diabetes mellitus. It primarily decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization.
| Metabolism | Metformin undergoes minimal hepatic metabolism; approximately 90% is excreted unchanged in the urine via tubular secretion. It is not metabolized by cytochrome P450 enzymes. |
| Excretion | Primarily renal excretion (70% unchanged), with 20% fecal elimination via biliary secretion; 10% metabolized. |
| Half-life | Terminal elimination half-life of 14 hours (range 12-16 h); clinically, steady-state achieved after 3 days. |
| Protein binding | 98% bound to albumin. |
| Volume of Distribution | Vd 0.8 L/kg; indicates extensive tissue distribution with accumulation in lung and liver. |
| Bioavailability | Oral bioavailability 60% due to first-pass metabolism. |
| Onset of Action | Oral: 1-2 hours; intravenous: within 5 minutes. |
| Duration of Action | 8-12 hours for oral dose; 6-8 hours for intravenous dose; prolonged in hepatic impairment. |
| Molecular Weight | 325.41 |
Locametz (gallium Ga 68 gozetotide) is administered intravenously at a dose of 3-5 mCi (110-185 MBq) as a single injection for PET imaging. No repeated dosing schedule is defined.
| Dosage form | POWDER |
| Renal impairment | No formal renal dose adjustment is required; however, in patients with severe renal impairment (eGFR <30 mL/min/1.73m²), the imaging quality may be reduced due to altered clearance. |
| Liver impairment | No specific dose adjustment is needed for hepatic impairment based on Child-Pugh classification. |
| Pediatric use | Pediatric dosing is not established; safety and efficacy in patients under 18 years have not been studied. |
| Geriatric use | No specific dose adjustment is recommended for elderly patients; however, caution is advised due to higher prevalence of renal impairment and comorbidities. |
| 1st trimester | No adequate studies in pregnant women; animal reproduction studies have shown fetal harm. Use only if potential benefit justifies risk to fetus. Avoid in first trimester due to risk of teratogenicity. |
| 2nd trimester | Use only if clearly needed, weighing potential benefits against risks. May cause fetal harm based on animal data. |
| 3rd trimester | Avoid use in third trimester due to risk of adverse effects on the fetus (e.g., oligohydramnios, renal impairment). Discontinue if pregnancy is detected. |
Clinical note
Comprehensive clinical and safety monograph for LOCAMETZ (LOCAMETZ).
| Placental transfer | Crosses placenta; detectable in fetal plasma and amniotic fluid. |
| Breastfeeding | Excreted in breast milk in small amounts; monitor infant for potential adverse effects (e.g., drowsiness, feeding problems). Use with caution and only if clearly indicated. |
■ FDA Black Box Warning
Lactic acidosis is a rare but serious metabolic complication that can occur due to metformin accumulation. Risk factors include renal impairment, concomitant cardiovascular collapse, acute myocardial infarction, sepsis, hepatic impairment, and excessive alcohol intake. Discontinue metformin immediately if lactic acidosis is suspected.
| Serious Effects |
Hypersensitivity to Locametz or any excipientSevere renal impairment (CrCl < 30 mL/min)Concomitant use with strong CYP3A4 inducersLactation period (risk outweighs benefit)
| Precautions | Lactic acidosis risk: assess renal function before starting and annually; discontinue if renal impairment or acute conditions develop., Monitor renal function; avoid in patients with eGFR <30 mL/min/1.73 m²., Hypoglycemia risk when used with insulin or insulin secretagogues., Vitamin B12 deficiency: monitor hematologic parameters annually., Temporary discontinuation for radiologic studies with iodinated contrast or surgical procedures., Avoid in acute conditions that may compromise renal function (e.g., dehydration, severe infection). |
| Food/Dietary |
Loading safety data…
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | Locametz (lutetium Lu 177 vipivotide tetraxetan) is a radiopharmaceutical. In pregnancy, radiation exposure poses significant fetal risk. First trimester: high risk of teratogenesis including CNS and cardiac defects. Second and third trimesters: increased risk of fetal growth restriction, microcephaly, and childhood malignancies. Use is contraindicated in pregnancy. |
| Fetal Monitoring | Monitor complete blood counts (CBC), renal function (serum creatinine, eGFR), and liver function tests (ALT, AST, bilirubin) at baseline and periodically. Assess for signs of myelosuppression. In pregnancy, if unavoidable, perform serial fetal ultrasounds and consider fetal dosimetry. |
| Fertility Effects | Radiation exposure may cause gonadal damage and impair fertility. In males, oligospermia or azoospermia; in females, ovarian failure and premature menopause. Long-term reproductive function may be permanently compromised. |
| No clinically significant food interactions for topical LOCAMETZ. Avoid ingesting the product. |
| Clinical Pearls | LOCAMETZ is a topical corticosteroid; avoid use on face, groin, axillae, or under occlusion due to increased absorption. Do not use for >2 weeks continuously. Monitor for signs of skin atrophy or systemic effects if applied to large areas. |
| Patient Advice | Apply a thin layer to affected skin only, not to healthy skin. · Do not cover treated area with bandages or dressings unless directed by doctor. · Wash hands after applying unless treating hands. · Avoid contact with eyes, mouth, and open wounds. · Do not use for longer than prescribed; report worsening or no improvement after 1 week. |